| 摘要 |
The present invention relates to an [18F]fluoromethyl group-introduced radiotracer for positron emission tomography for targeting brain neuroinflammation, a synthesis thereof, and a method for evaluating biological results using the same. In the present invention, a fluoromethyl group-introduced fluorine-18 labeled radiotracer was prepared by introducing [18F]fluoroiodomethane, in which a prosthetic group diiodomethane is labeled with fluorine-18, into PBR28-OH through two stages, or substituting fluorine-18 using a triazolium triflate precursor in one stage at high yield. It was confirmed that, as a result of comparison and evaluation with exiting known [11C]PBR28 in view of in vitro binding affinity, fat affinity, and pharmacodynamic characteristics in a brain neuroinflammation model, the fluoromethyl group-introduced fluorine-18 labeled radiotracer had similar binding affinity and fat affinity to [11C]PBR28. Further, it was confirmed from the PET image comparison and evaluation in the brain neuroinflammation model that the fluoromethyl group-introduced fluorine-18 labeled radiotracer exhibited excellent selective/specific absorption in the inflammatory region more quickly and had high stability at the brain neuroinflammation site. According to the present invention, with respect to the synthesis of the novel fluoromethyl group-introduced fluorine-18 labeled radiotracer for PET targeting brain neuroinflammation and the diagnosis of brain neuroinflammation diseases, fluorine-18 having a relatively longer half-life than [11C]PBR28 was capable of being excellently labeled through the minimum structural change, and its excellent selective and specific imaging and pharmacodynamic advantages were verified, and thus a useful radiotracer for PET targeting brain neuroinflammation can be expected. |
